Santacruzamate A

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Chemical Structure| 1477949-42-0 同义名 : CAY-10683
CAS号 : 1477949-42-0
货号 : A172133
分子式 : C15H22N2O3
纯度 : 99%+
分子量 : 278.347
MDL号 : N/A
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(377.23 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

5%DMSO+30%PEG300+5%TW80+water 10 mg/mL

生物活性
靶点

  • HDAC2

    HDAC2, IC50:119 pM
描述 Histone deacetylases (HDACs) are a class of enzymes that remove acetyl groups from specific lysine residues on core histones, thereby regulating gene transcription via histone and chromatin structure modifications[2]. Santacruzamate A (CAY10683) is a picomolar level selective inhibitor of HDAC2, a Class I HDAC, with relatively little inhibition of HDAC4 or HDAC6, both Class II HDACs[3]. Pretreatment with Santacruzamate A resulted in a significant reduction in Aβ protein fragment 25–35 (Aβ25–35) -induced toxicity, with 2 µM STA showing the strongest protective effects in PC12, STA also rescues cognitive deficits in APPswe/PS1dE9 mice by enhancing ER stress tolerance[4]. Compared with the normal group, expression levels of inflammatory cytokine IL-1β and TNF-α were significantly increased in LPS activated BV2 microglial cells (P<0.05),CAY10683 could inhibit expression levels of inflammatory cytokine TNF-α and IL-1β in LPS activated BV2 microglial cells and LPS induced mice neuroinflammation[5]. CAY10683 improves histological and functional changes in ALF model. Compared with control group, LPS/D-GalN induced massive apoptosis of rat intestinal tissues and NCM460 cells (P<0.05), and the apoptosis rate was significantly reduced after CAY10683 treatment (P<0.05). The expression of Bax was increased significantly in the model groups (P<0.05), and reduced with the treatment of CAY10683 (P<0.05). Compared with the model group, CAY10683 inhibits mitochondrial apoptosis in intestinal tissues and NCM460 cells (P<0.05)[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.96mL

3.59mL

1.80mL

35.93mL

7.19mL

3.59mL
参考文献

[1]Pavlik CM, Wong CY, et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp. J Nat Prod. 2013 Nov 22;76(11):2026-33.

[2]Hengyu Zhou, Pharmacological or transcriptional inhibition of both HDAC1 and 2 leads to cell cycle blockage and apoptosis via p21Waf1/Cip1 and p19INK4d upregulation in hepatocellular carcinoma, Cell Prolif.2018 Jun;51(3):e12447.

[3]Christopher M Pavlik,et al. Santacruzamate A, a potent and selective histone deacetylase inhibitor from the Panamanian marine cyanobacterium cf. Symploca sp, J Nat Prod.2013 Nov 22;76(11):2026-33.

[4] Lei Chen,et al. Santacruzamate A Ameliorates AD-Like Pathology by Enhancing ER Stress Tolerance Through Regulating the Functions of KDELR and Mia40-ALR in vivo and in vitro . Front Cell Neurosci. 2019 Mar 4;13:61.

[5] Fang‑Zhou Jiao,et al. Histone Deacetylase 2 Inhibitor CAY10683 Alleviates Lipopolysaccharide Induced Neuroinflammation Through Attenuating TLR4/NF-κB Signaling Pathway,Neurochem Res. 2018 Jun;43(6):1161-1170.

[6] Yang Liu,et al. HDAC2 inhibitor CAY10683 reduces intestinal epithelial cell apoptosis by inhibiting mitochondrial apoptosis pathway in acute liver failure, Histol Histopathol. 2019 Oct;34(10):1173-1184.